oral BET inhibitor

4.5 mg QD, phase I/II for cancer

from bromodomain-focused HTS, SBDD

Journal of Medicinal Chemistry

Bristol Myers Squibb


The BMS BET inhibitor, BMS-986158, is in a Ph. I/IIa trial in advanced cancers. During the optimization of the molecule from a carbazole hit, the authors employed a bold scaffold-hopping…

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